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Sparfloxacin, Uses, Dosage, Side effects, Interactions, Pregnancy

Sparfloxacin is a fluoroquinolone antibiotic that inhibits bacterial DNA gyrase, thereby inhibiting DNA replication and transcription. Sparfloxacin was withdrawn from the U.S. market due to a high incidence of phototoxicity.

Sparfloxacin is a fluoroquinolone antibiotic used in the treatment of bacterial infections. Sparfloxacin exerts its antibacterial activity by inhibiting DNA gyrase, a bacterial topoisomerase. DNA gyrase is an essential enzyme which controls DNA topology and assists in DNA replication, repair, deactivation, and transcription.

Mechanism of action of Sparfloxacin

Sparfloxacin is a synthetic fluoroquinolone broad-spectrum antimicrobial agent in the same class as ofloxacin and norfloxacin. Sparfloxacin has in vitro activity against a wide range of gram-negative and gram-positive microorganisms. Sparfloxacin exerts its antibacterial activity by inhibiting DNA gyrase, a bacterial topoisomerase. DNA gyrase is an essential enzyme which controls DNA topology and assists in DNA replication, repair, deactivation, and transcription. Quinolones differ in chemical structure and mode of action from (beta)-lactam antibiotics. Quinolones may, therefore, be active against bacteria resistant to (beta)-lactam antibiotics. Although cross-resistance has been observed between sparfloxacin and other fluoroquinolones, some microorganisms resistant to other fluoroquinolones may be susceptible to sparfloxacin. In vitro tests show that the combination of sparfloxacin and rifampin is antagonistic against Staphylococcus aureus.

The bactericidal action of sparfloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV, which are required for bacterial DNA replication, transcription, repair, and recombination.

Indications of Sparfloxacin

For the treatment of adults with the following infections caused by susceptible strains microorganisms: community-acquired pneumonia (caused by Chlamydia pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Mycoplasma pneumoniae, or Streptococcus pneumoniae) and acute bacterial exacerbations of chronic bronchitis (caused by Chlamydia pneumoniae, Enterobacter cloacae, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Staphylococcus aureus, or Streptococcus pneumoniae).
Treatment of radiologically confirmed community acquired pneumonia which has failed to respond to conventional therapy
Community-acquired pneumonia
Bacterial Infection
Bronchitis
Acute bacterial exacerbations of chronic bronchitis
Leprosy, Borderline
Leprosy, Lepromatous
Pneumonia
Acne,
Burns,
Conjunctivitis,
Cystitis,
Dysenteries,
Folliculitis,
Impetigo,
Otitis media,
Prostatitis,
Pyelonephritis,
Respiratory tract infections,
Sinusitis,
Superficial infections,
Surgical infections,
Tonsillitis,
Urethritis
Travelers’ Diarrhea
Ulcerative keratitis
Uncomplicated Cystitis
Bronchitis
Campylobacter Gastroenteritis
Cervicitis
Chancroid
Chlamydia Infection
Epididymitis, Non-Specific
Epididymitis, Sexually Transmitted
Joint Infection
Kidney Infections

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Contra-Indications of Sparfloxacin

Subacute cutaneous lupus erythematosus
Systemic lupus erythematosus
use should be avoided in pregnant or lactating women, and in children with developing teeth because they may result in permanent staining (dark yellow-gray teeth with a darker horizontal band that goes across the top and bottom rows of teeth), and possibly affect the growth of teeth and bones.
Allergy
Avoid taking this medicine if you have a known allergy to it or any other fluoroquinolones.
Tendinitis or tendon rupture
Avoid if you have a past history of tendinitis or tendon rupture after using this medicine.
Myasthenia Gravis

Avoid if you have a past history of myasthenia gravis or family history of myasthenia gravis.

Dosage of Sparfloxacin

Strengths : 100 mg, 200 mg, 400 mg

Sparfloxacin’s dosage details are as follows

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
100 to 200 mg	150 (150)	12 hourly	PO	Maintenance.
400 mg	400 (400)	24 hourly	PO	Initially.
Paedriatic Dosage (20kg)
				Not recommended in this age group
Neonatal Dosage (3kg)
				Not recommended in this age group

Bronchitis

Acute bacterial exacerbations of chronic bronchitis

400 mg orally once as a loading dose, followed by 200 mg orally once a day thereafter for a total of 10 days.

Leprosy – Borderline

200 mg orally daily.

Pneumonia

Community-acquired pneumonia

400 mg orally once as a loading dose, followed by 200 mg orally once a day thereafter for a total of 10 days.

Side Effects of Sparfloxacin

The most common

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More common

Abdominal or stomach pain, discomfort, or tenderness
chills or fever
a headache, severe and throbbing
joint or back pain
muscle aching or cramping
muscle pains or stiffness
chest pressure or squeezing pain in the chest
excessive sweating
feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
sudden tingling or coldness in an arm or leg
sudden slow or difficult speech
sudden drowsiness or need to sleep
fast breathing
sharp pain when taking a deep breath
fast or slow heartbeat
coughing up blood
decreased amount of urine

Rare

Drug Interactions of Sparfloxacin

Sparfloxacin may interact with following drugs, supplements, & may change the efficacy of drugs

antacids that contain aluminum, calcium, or magnesium
birth control medications
bismuth subsalicylate
calcium supplements
digoxin
Rosuvastatin
Duloxetine
Albuterol
Topiramate
Carbamazepine
Vitamin D3 (cholecalciferol)
Alprazolam
Cetirizine
insulin
iron supplements
penicillin
vitamin A derivatives (e.g. isotretinoin)
warfarin
zinc sulfate or gluconate

Pregnancy & Lactation of Sparfloxacin

FDA Pregnancy Category C

Pregnancy

Sparfloxacin has been assigned to pregnancy category C by the FDA. High-dose animal studies revealed no evidence of teratogenicity. However, when studied in rats at maternally toxic doses (9.3 times the maximum human dose based on mg/m2) there was an increased incidence of fetuses with ventricular septal defects. This event was not observed in monkeys or rabbits at maternally toxic doses. There are no controlled data in human pregnancy.

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Lactation

Sparfloxacin is excreted into human milk. Cartilage erosion and arthropathy have been reported in immature animals giving rise to concern over toxic effects in the developing joints of nursing infants. The manufacturer recommends that due to the potential for serious adverse reactions in nursing infants, a decision should be made to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.